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  • Title: Identification of nitroimidazole-oxime derivatives targeting the polo-box domain of polo-like kinase 1.
    Author: Sun J, Liu HY, Xu RF, Zhu HL.
    Journal: Bioorg Med Chem; 2017 Dec 15; 25(24):6581-6588. PubMed ID: 29100732.
    Abstract:
    Recent progress in the development of small molecular skeleton-derived polo-like kinase (PLK1) catalytic domain (KD) inhibitors has led to the synthesis of multiple ligands with high binding affinity. However, few systematic analyses have been conducted to identify key PLK1-PBD domain and characterize their interactions with potent PLK1 inhibitors. Therefore, we designed a series of PLK1-PBD inhibitors with an in silico scaffold modification strategy. A docking simulation combined with a primary screen in vitro were performed to filter for the lead compound, which was then substituted, synthesized and evaluated by a variety of bioassays. The biological profile of 4v suggests that this compound may be developed as a potential anticancer agent.
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